Art. -Nr.: HY-B0251

Eplerenone

Name: Eplerenone
Brand: MedChemExpress
SKU: HY-B0251
Price: 56.00 USD
Availability: InStock
Rating: 5 (8 reviews)

(Synonyms: Epoxymexrenone)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC₅₀ value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).

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Reinheit : 99.81%
CAS. Nr.: 107724-20-9
Formel: C₂₄H₃₀O₆
Molecular Weight:414.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Eplerenone Chemical Structure

CAS. Nr.: 107724-20-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.081 μM (human mineralocorticoid receptor) ^[2]

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	>5000 nM Compound: 1	Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay	[PMID: 20408553]
COS-1	IC₅₀	1300 nM Compound: Eplerenone	Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay	[PMID: 22074142]
COS-1	IC₅₀	1300 nM Compound: Eplerenone	Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay	[PMID: 25187277]
HEK293	IC₅₀	2600 nM Compound: Eplerenone	Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting	[PMID: 22074142]
Huh-7	IC₅₀	135 nM Compound: 1	Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay	[PMID: 20408553]
Huh-7	IC₅₀	122 nM Compound: 1	Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay	[PMID: 20672820]
Huh-7	IC₅₀	122 nM Compound: eplerenone	Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay	[PMID: 20672822]

In Vitro

Eplerenone inhibits the human mineralocorticoid receptor with IC₅₀ value of 0.081 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eplerenone (oral, 200 mg/kg/day for 3 months) significantly reduces oxidative stress and atherosclerosis progression in atherosclerotic apolipoprotein edeficient (EO) mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Atherosclerotic apolipoprotein Edeficient (EO) mice^[3]
Dosage:

200 mg/kg
Administration:

oral, 200 mg/kg/day for 3 months
Result:

Significantly decreased systolic and diastolic blood pressure by 12% and 11%, respectively.
Decreased serum susceptibility to lipid peroxidation by as much as 26%, and increased serum paraoxonase activity by 28%.
Reduced levels of lipid peroxides, and significantly reduced macrophage oxidation of low-density lipoprotein (LDL) and superoxide ion release.
Significantly reduced the atherosclerotic lesion area.

Related Protocols :

Research Protocol for Cardiovascular Diseases

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 107724-20-9
Appearance Solid
Molecular Weight 414.49
Formel C₂₄H₃₀O₆
Color White to off-white
SMILES

O=C(CC1)O[C@@]21CC[C@@]3([H])[C@]4([H])[C@H](C(OC)=O)CC5=CC(CC[C@]5(C)[C@@]46[C@H](O6)C[C@@]32C)=O
Synonyms

Epoxymexrenone
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All Histological Imaging/StainingWBCell Imaging/StainingCell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

Br J Pharmacol

Protopanaxadiol alleviates neuropathic pain by spinal microglial dynorphin A expression following glucocorticoid receptor activation. [Abstract]

2021 Aug;178(15):2976-2997. PMID: 33786848
Biochem Pharmacol

Tspan4+ fibroblasts facilitate the development of NECSO in myocardial ischemia reperfusion through migrasomes-mediated Tnf-α autocrine and cardiomyocytes aldosterone generation. [Abstract]

2026 Jul:249:117928. PMID: 41887336
Mol Med Rep

Age‑related changes in mineralocorticoid receptors in rat hearts. [Abstract]

2020 Sep;22(3):1859-1867. PMID: 32582979

Eplerenone purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2020 Sep;22(3):1859-1867. [Abstract]

Eplerenone (1 μM). Mmunoblotting and semi-quantification of p16, p21, p53 and NADP subunits, p47-phox, p67-phox and gp91-phox expression in H9C2 cells. Protein expression levels were normalized to GAPDH.
Sci Rep

Activation/inactivation of Tregs mediated by Kv1.3 potassium channels synergistically with exosome secretion to regulate myocardial fibrosis. [Abstract]

2025 Dec 1;15(1):45756. PMID: 41326524

Eplerenone purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Dec 1;15(1):45756. [Abstract]

Eplerenone (200 mg/kg/day). Hematoxylin and eosin (H&E) staining was performed to assess cardiomyocyte arrangement and inflammatory infiltration.
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Theriogenology

Aldosterone regulates in vitro maturation of porcine oocytes derived from small follicles via Wnt/ β-catenin. [Abstract]

2026 Apr 15:255:117836. PMID: 41564797

Eplerenone purchased from MedChemExpress. Usage Cited in: Theriogenology. 2026 Apr 15:255:117836. [Abstract]

Representative images of cumulus cell expansion and oocytes with or without polar bodies in the control group and groups treated with different concentrations of EPL (Eplerenone) after in vitro maturation (IVM).
Otol Neurotol

Cortisol Sensitizes Cochlear Hair Cells to Gentamicin Ototoxicity Via Endogenous Apoptotic Pathway. [Abstract]

2024 Jan 1;45(1):e49-e56. PMID: 38085767

Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]

Cells were treated with cortisol (50 μmol/l) in combination with different concentrations of RU486 or Eplerenone for 24 hours.

Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]

HEI-OC1 cells were treated with 50 μmol/l cortisol in combination with 0.1 nmol/l RU486 or 1 μmol/l Eplerenone for 24 hours and then treated with 50 mmol/l GM for 24 hours. apoptosis was assessed by flow cytometry using Annexin V and PI staining kit.
Research Square Preprint

2021 Apr.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 5 mg/mL (12.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4126 mL

12.0630 mL

24.1260 mL

5 mM

0.4825 mL

2.4126 mL

4.8252 mL

10 mM

0.2413 mL

1.2063 mL

2.4126 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (297 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Myron H Weinberger, et al. Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens. 2002 Aug;15(8):709-16. [Content Brief]

[2]. Dhillon, S., Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms. Drugs, 2013. 73(13): p. 1451-62. [Content Brief]

[3]. Shlomo Keidar, et al. Effect of eplerenone, a selective aldosterone blocker, on blood pressure, serum and macrophage oxidative stress, and atherosclerosis in apolipoprotein E-deficient mice. J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4126 mL	12.0630 mL	24.1260 mL	60.3151 mL
	5 mM	0.4825 mL	2.4126 mL	4.8252 mL	12.0630 mL
	10 mM	0.2413 mL	1.2063 mL	2.4126 mL	6.0315 mL

Bioz

Keywords

Eplerenone

8 Cited Publications

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Eplerenone

Publications Citing Use of MedChemExpress (MCE) Eplerenone

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen